公开(公告)号：US20060116379A1

公开(公告)日：2006-06-01

申请号：US11274308

申请日：2005-11-16

申请人： Tomoyuki Ogawa ,  Kaoru Seno ,  Kohji Hanasaki ,  Minoru Ikeda ,  Takashi Ono

发明人： Tomoyuki Ogawa ,  Kaoru Seno ,  Kohji Hanasaki ,  Minoru Ikeda ,  Takashi Ono

IPC分类号： A61K31/503 ,  A61K31/498 ,  C07D487/04

CPC分类号： C07D403/12 ,  C07D209/12 ,  C07D209/22 ,  C07D209/24 ,  C07D209/42 ,  C07D487/04

摘要： A compound represented by the general formula: wherein R20 is —CH2COOH and the like; R21 is —COCONH2 and the like; R22 is C4-C6 alkyl; and the like; R23 is —CH2—R18 wherein R18 is aryl and the like; R24 is hydrogen or C1-C6 alkyl and the like; an optical active compound, a prodrug thereof, or a pharmaceutically acceptable salt, or a solvate having type X sPLA2 inhibitory effect was found.

摘要翻译： 由以下通式表示的化合物：其中R 20为-CH 2 COOH等; R 21是-COCONH 2 N 2等; R 22是C 4 -C 6烷基; 等等; R 23是-CH 2 - ，其中R 18是芳基等; R 24是氢或C 1 -C 6烷基等; 发现光学活性化合物，其前体药物或药学上可接受的盐，或具有X sPLA 2抑制作用的溶剂化物。

公开(公告)号：US07026318B2

公开(公告)日：2006-04-11

申请号：US10311282

申请日：2001-06-27

申请人： Tomoyuki Ogawa ,  Kaoru Seno ,  Kohji Hanasaki ,  Minoru Ikeda ,  Takashi Ono

发明人： Tomoyuki Ogawa ,  Kaoru Seno ,  Kohji Hanasaki ,  Minoru Ikeda ,  Takashi Ono

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/495 ,  A61K31/50 ,  C07D241/36

CPC分类号： C07D403/12 ,  C07D209/12 ,  C07D209/22 ,  C07D209/24 ,  C07D209/42 ,  C07D487/04

摘要： A compound represented by the general formula: wherein R20 is —CH2COOH and the like; R21 is —COCONH2 and the like; R22 is C4–C6 alkyl; and the like; R23 is —CH2—R18 wherein R18 is aryl and the like; R24 is hydrogen or C1–C6 alkyl and the like; an optical active compound, a prodrug thereof, or a pharmaceutically acceptable salt, or a solvate having type X sPLA2 inhibitory effect was found.

摘要翻译： 由以下通式表示的化合物：其中R 20为-CH 2 COOH等; R 21是-COCONH 2 N 2等; R 22是C 4 -C 6烷基; 等等; R 23是-CH 2 - ，其中R 18是芳基等; R 24是氢或C 1 -C 6烷基等; 发现光学活性化合物，其前体药物或药学上可接受的盐，或具有X sPLA 2抑制作用的溶剂化物。

公开(公告)号：US06703385B1

公开(公告)日：2004-03-09

申请号：US10031443

申请日：2002-01-22

申请人： Mitsuaki Ohtani ,  Masahiro Fuji ,  Makoto Adachi ,  Tomoyuki Ogawa

发明人： Mitsuaki Ohtani ,  Masahiro Fuji ,  Makoto Adachi ,  Tomoyuki Ogawa

IPC分类号： A61K3133

CPC分类号： C07D471/04

摘要： The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is COCONH2 or the like; Q1 is a nitrogen atom or C—R4; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; R21 and R22 are hydrogen atoms or the like; X is —CR23R24— or the like wherein R23 and R24 are hydrogen atoms or the like; Y is —CR25R26— or the like wherein R25 and R26 are hydrogen atoms or the like; Z is CH2 or the like; a broken line ( - - - ) represents the presence or absence of a bond, its prodrug, their pharmaceutically acceptable salt, or solvate thereof.

摘要翻译： 本发明提供具有sPLA2抑制活性的化合物。式（I）表示的化合物：其中R 1为（a）C 1至C 20烷基，C 2至C 20烯基，C 2至C 20炔基，碳环基，杂环基 或类似物; R 2是COCONH 2等; Q 1是氮原子或C-R 4; R 3和R 4之一是 - （L 2） - （酸性基团）其中L 2是与酸基连接的基团和连接基团的长度为1至5个原子，以及 另一个是氢原子; R 21和R 22是氢原子等; X是-CR 23 R 24 - 等，其中R 23和R 24是氢原子等; Y是-CR 25 R 26 - 等，其中R 25和R 26是氢原子等; Z是CH 2等; 虚线（ - - - ）表示键的存在或不存在，其前体药物，其药学上可接受的盐或溶剂合物。